Abstract

This chapter elaborates the therapeutic category, synthesis, ultraviolet spectrum, optical rotation, thermoanalytical behavior, stability, and determination in biological matrices of timolol maleate. Timolol maleate is a beta adrenergic blocker that is nonselective between beta 1 and beta 2 adrenergic receptors. Both the proton and C 13 nuclear magnetic resonance (NMR) spectra are consistent with the timolol maleate structure. Timolol maleate, having one chiral carbon, is optically active. The levorotatory enantiomer is the biologically active form. The solubilities of timolol maleate in a variety of solvents at room temperature are presented in this chapter. Timolol maleate may be identified through the use of elemental analysis. Aqueous solutions of timolol maleate have also been shown to be susceptible to degradation when exposed to intense ultraviolet radiation. Biological testing of synthetic samples of Metabolites I, II, and III shows only Metabolite II to have significant 6-adrenergic blocking activity.

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